AMLODIPINE BESYLATE
  • AMLODIPINE BESYLATE

  • (Generic for NORVASC)
  • QTY 30 • 10 MG • Tablet • Near 77381

AMLODIPINE (am LOE di peen) is a calcium-channel blocker. It affects the amount of calcium found in your heart and muscle cells. This relaxes your blood vessels, which can reduce the amount of work the heart has to do. This medicine is used to lower high blood pressure. It is also used to prevent chest pain.

AMLODIPINE BESYLATE Pediatric Monographs
  • General Administration Information
    For storage information, see the specific product information within the How Supplied section.

    Route-Specific Administration

    Oral Administration
    -May administer without regard to meals.
    Oral Liquid Formulations
    Oral suspension
    -Shake well before using.
    -Measure with a calibrated oral syringe.
    -Storage: Keep in refrigerator (36 to 46 degrees F [2 to 8 degrees C]).

    Extemporaneous Compounding-Oral
    Extemporaneous 1mg/mL amlodipine oral suspension preparation:
    NOTE: The extemporaneous preparation of amlodipine is not approved by the FDA.
    -With a mortar and pestle, grind twenty-four 5 mg amlodipine tablets to a fine powder.
    -In a separate container, mix 60 mL of Ora-Sweet with 60 mL of Ora-Plus to make the base solution. Shake well.
    -Add a small amount of base solution to amlodipine powder to form a paste. Add geometric amounts of the base solution while mixing well, leaving enough base solution to rinse the mortar after the mixture is transferred to a graduated cylinder.
    -Transfer mixture to a graduated cylinder and add the additional base solution to make a total volume of 120 mL. The final concentration is 1 mg/mL.
    -Storage: Place in an amber plastic bottle. Shake well before each use. This oral suspension is stable for 90 days refrigerated or up to 56 days when stored at room temperature (approximately 25 degrees C or 77 degrees F).

    Most adverse reactions to amlodipine are mild to moderate in severity and related to the drug's peripheral vasodilatory effect. Amlodipine 2.5 or 5 mg/day PO was well tolerated in a randomized, double-blind, placebo-controlled study of 268 hypertensive pediatric patients 6 years and older. In this trial, 6 patients were withdrawn from amlodipine therapy due to drug-related adverse events. Adverse effects are similar to those observed for adults.

    Severe headache (3%) and peripheral edema (2.3% to 4.3%) were the most commonly reported adverse reactions in a placebo-controlled study of 268 hypertensive pediatric patients. Asthenia, dizziness, and epistaxis were among the most common mild to moderate adverse reactions thought to be treatment-related. In the adult CAMELOT and PREVENT studies, peripheral edema was the most commonly reported adverse reaction, occurring in 32.4% and 13.6% of patients, respectively. In adult clinical trials, edema (1.8% to 14.6%), dizziness (1.1% to 3.4%), palpitations (0.7% to 4.5%), and flushing (0.7% to 4.5%) were dose-related adverse reactions. Edema, palpitations, and flushing appear to occur more frequently in women. Adverse reactions that do not appear to be dose-related include fatigue (4.5%), asthenia (less than 2%), epistaxis (less than 1%), and drowsiness (1.3% to 1.6%).

    Jaundice and elevated hepatic enzymes (mostly consistent with cholestasis or hepatitis), in some cases severe enough to require hospitalization, have been reported with postmarketing experience. Discontinue amlodipine in patients who develop jaundice and begin appropriate therapy. Pancreatitis has also been reported rarely (less than 1%).

    Leukopenia and thrombocytopenia were reported in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience. Gynecomastia has been infrequently reported with postmarketing experience; however, a causal relationship is uncertain.

    Peripheral neuropathy, postural dizziness, paresthesias, tremor, and vertigo have been reported in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Ventricular arrhythmia was reported in 1 patient (0.3%) receiving amlodipine in a placebo-controlled study of 268 hypertensive pediatric patients. Arrhythmia exacerbation (including ventricular tachycardia and atrial fibrillation), bradycardia, syncope, chest pain (unspecified), peripheral ischemia, sinus tachycardia, and vasculitis have been reported in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; however, a causal relationship has not been established. Since the peripheral vasodilation induced by amlodipine is gradual in onset, acute hypotension has rarely been reported after oral administration. Nonetheless, exercise caution when administering amlodipine, as with any other peripheral vasodilator, to patients at risk for hypotension.

    Hypoesthesia, insomnia, nervousness or anxiety, depression, abnormal dreams (e.g., nightmares), and depersonalization have been reported in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; however, a causal relationship has not been established.

    Muscle cramps were reported in 2% or less of amlodipine-treated patients in clinical trials. Back pain, hot flashes, malaise, pain, rigors (chills), weight gain, weight loss, arthralgia, arthrosis, and myalgia occurred in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established. Based on postmarketing reports, there is a possible association between amlodipine and extrapyramidal disorder.

    Dyspnea was reported in 2% or less of amlodipine-treated patients during clinical trials.

    Xerostomia (0.3%) and vomiting (0.3%) were classified as severe adverse reactions in a placebo-controlled study of 268 hypertensive pediatric patients. Abdominal pain was among the most common mild to moderate adverse reactions thought to be treatment-related. Abdominal pain (1.6%) and nausea (2.9%) were reported in adult clinical trials, and not considered dose-related. Xerostomia, anorexia, constipation, diarrhea, dysphagia, gingival hyperplasia, flatulence, and vomiting occurred in less than 1% of patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Conjunctivitis, diplopia, visual impairment (abnormal vision), ocular pain, and tinnitus have been reported in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Pruritus and rash were reported in 2% or less of patients during clinical trials. Angioedema, allergic reactions, erythema, erythema multiforme, maculopapular rash, purpura, and diaphoresis occurred in less than 1% of patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Increased urinary frequency, micturition disorder, and nocturia occurred in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Hyperglycemia and thirst (polydipsia) occurred in less than 1% of amlodipine-treated patients in controlled clinical trials, open trials, or marketing experience; a causal relationship has not been established.

    Amlodipine is contraindicated in patients with known hypersensitivity to amlodipine.

    Systematic hypotension is possible with amlodipine, particularly in patients with aortic stenosis. Because of the gradual onset of action of amlodipine, acute hypotension is unlikely.

    Use amlodipine with caution in patients with hepatic disease; dosage adjustment with slow dose titration is recommended. Amlodipine is extensively metabolized by the liver and elimination half-life is prolonged in patients with hepatic impairment.

    Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of amlodipine, particularly in adult patients with severe obstructive coronary artery disease.

    Description: Amlodipine is an oral calcium-channel blocker used for the treatment of hypertension. It is a potent peripheral vasodilator, similar to nifedipine and other members of the dihydropyridine class, although amlodipine has the longest half-life of the group. Although FDA-approved labeling recommends once-daily dosing of amlodipine, younger children may benefit from twice daily dosing due to faster clearance and higher weight-based dosage requirements relative to older children. In adult patients, amlodipine is considered less effective than ACE inhibitors or AII-receptor antagonists in slowing the progression of renal disease in patients with diabetic nephropathy or hypertensive renal disease. Amlodipine is FDA-approved in pediatric patients as young as 6 years of age.

    For the treatment of hypertension:
    Oral dosage:
    Children 1 to 5 years*: 0.1 mg/kg/dose PO once daily initially; Max: 0.6 mg/kg/dose, up to 5 mg/dose is recommended by pediatric hypertension guidelines. However, initial doses ranging from 0.05 to 0.2 mg/kg/day PO, given in 1 or 2 divided doses, have been recommended. Max reported doses = 0.3 to 0.6 mg/kg/day (up to 10 to 20 mg/day). Adult Max dose: 10 mg/day. Adjust dose every 5 to 7 days; it may require several weeks for the maximum hypotensive effect to fully manifest. Younger children require higher doses per kg of body weight relative to older children and may benefit from twice daily dosing in some cases.
    Children and Adolescents 6 to 17 years: 2.5 to 5 mg PO once daily; Max: 5 mg/day. Some investigators have reported initial doses of 0.05 to 0.3 mg/kg/day PO with a Max of 0.34 mg/kg/day (up to 10 mg/day) or 0.6 mg/kg/day (up to 20 mg/day). Adult Max: 10 mg/day. Adjust dose every 5 to 7 days; it may require several weeks for the maximum hypotensive effect to fully manifest. Younger children require higher doses per kg of body weight relative to older children and may benefit from twice daily dosing in some cases.

    Maximum Dosage Limits:
    -Neonates
    Safety and efficacy have not been established.
    -Infants
    Safety and efficacy have not been established.
    -Children
    1 to 5 years: Safety and efficacy have not been established; however, doses up to 0.6 mg/kg/day PO (Max: 20 mg/day) have been reported.
    6 to 12 years: 5 mg/day PO is the maximum dosage per FDA-approved labeling; however, doses up to 0.6 mg/kg/day PO (Max: 20 mg/day) have been reported.
    -Adolescents
    5 mg/day PO is the maximum dosage per FDA-approved labeling; however, doses up to 0.6 mg/kg/day PO (Max: 20 mg/day) have been reported.

    Patients with Hepatic Impairment Dosing
    Specific guidelines for dosage adjustments in pediatric patients with hepatic impairment are not available. FDA-approved product labeling recommends an initial dosage reduction of 50% (2.5 mg PO once daily) in adults with hepatic insufficiency; adjust dosage based on clinical response.

    Patients with Renal Impairment Dosing
    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    *non-FDA-approved indication

    Monograph content under development

    Mechanism of Action: Amlodipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes. Serum calcium levels remain unchanged. Amlodipine inhibits this influx, and the resultant decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, resulting in dilation of the coronary and systemic arteries. As with other calcium-channel blockers of the dihydropyridine class, amlodipine exerts its effects mainly on arteriolar vasculature. It has no significant effect on sinus node function or cardiac conduction, nor does it possess negative inotropic effects at clinical doses. Because it has a gradual onset, reflex tachycardia does not occur, a side effect that is common with other peripheral vasodilators. Amlodipine therapy usually does not affect hemodynamic parameters in patients with normal ventricular function.

    Pharmacokinetics: Amlodipine is administered orally. Amlodipine is approximately 93% bound to plasma proteins. Amlodipine is extensively metabolized to inactive compounds by the liver with 10% of the parent compound and 60% of the inactive metabolites excreted in the urine. The terminal half-life is about 30 to 50 hours. Steady-state plasma concentrations of amlodipine are reached after 7 to 8 days of consecutive daily dosing.

    Affected cytochrome P450 isoenzymes and drug transporters: CYP3A4
    Amlodipine is a CYP3A4 substrate, and its metabolism may be affected by CYP3A4 inhibitors or inducers. Coadministration of erythromycin in healthy volunteers did not significantly change amlodipine systemic exposure; however, strong CYP3A4 inhibitors may increase amlodipine plasma concentrations to a greater extent.


    -Route-Specific Pharmacokinetics
    Oral Route
    After oral administration, amlodipine peak plasma concentrations are achieved between 6 to 12 hours. Oral bioavailability is estimated to be 64% to 90%; food does not significantly affect absorption. The exposure of amlodipine oral suspension is similar to that of the tablets.


    -Special Populations
    Pediatrics
    Children and Adolescents
    Weight-adjusted clearance and volume of distribution were similar to values observed in adults during clinical trials (n= 62; age range: 6 to 17 years). In another pharmacokinetic study, older children and adolescents with body weights similar to that of adults demonstrated similar pharmacokinetic parameters. However, children younger than 6 years demonstrated a weight-normalized clearance of 1 +/- 0.33 L/kg/hour compared to 0.63 +/- 0.36 L/kg/hour for those 6 to 12 years and 0.4 +/- 0.16 L/kg/hour for those 13 to 18 years. Amlodipine serum concentrations were similar whether amlodipine was dosed once or twice daily.

    Hepatic Impairment
    Amlodipine is extensively metabolized by the liver; clearance is decreased in patients with hepatic impairment. In these patients, the plasma elimination half-life is prolonged (56 hours) and the AUC is increased by 40% to 60%.

    Renal Impairment
    The pharmacokinetics of amlodipine are not significantly impacted by renal impairment.

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